Biologically active food supplement

ABSTRACT

A biologically active food supplement intended to increase the athletes&#39; muscle mass comprises Leuzea (or other medicinal plant containing ecdysteroids), male bee brood, ascorbic acid (Vitamin C). Vitamin E, and excipients (calcium stearate, talc, lactose) with the following ratio of components (mass %): Male bee brood 1-70; Leuzea 5-70; Ascorbic acid 1-70; Vitamin E 0.05-30; calcium stearate 0.92-0.95; talc 3-6; lactose—the rest.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application is a continuation in part of U.S. application Ser. No. 13/256,237 filed on Sep. 13, 2011, which is a U.S. National Stage application of International application no. PCT/RU2010/000098, claiming priority on Russian Federation application no. RU 2009109273 filed on Mar. 13, 2009, all of which are incorporated herein by reference in their entirely.

FIELD OF THE INVENTION

The invention relates to food industry, and specifically, to biologically active food additives, and is intended for increasing muscular weight in athletes and maintaining testosterone level, while providing anabolic, anticatabolic and potency enhancing effect.

BACKGROUND OF THE INVENTION

The best biostimulators and energetically rich products are the preparations developed based on bee hive products. The preparation “Tonus” is known, which was developed based on pollen and milk sugar (lactose) and approved by the Central Sanitary Administration under the President of the Russian Federation (RF) TU-64-02-06-244-91. This preparation is produced by “Biokor”. However, this preparation does not contain a polyvitamin complex or any vital microelements. Its effect on a human body is explained strictly by the presence of pollen, which could complicate the interpretation of biological activity of the “Tonus” as it becomes necessary to know precisely when the pollen was collected and from what plants. The closest prototypes to the invention in terms of the technical substance and achievable result are the natural polyvitamin complex Leveton (RU patent 2,066,963; Int. Cl. A23L001/076) and APILAR tablets (RU patent 2,233,666) based on drone brood.

According to the source RU 2,066,963, “Leveton contains pollen (pollen load), rhaponticum carthamoides, ascorbic acid, alpha-tocopherol acetate, propolis, calcium stearate, talc and lactose at the following ingredient ratio (wt. %): Pollen (pollen load): 50-51; Rhaponticum carthamoides: 10; Ascorbic acid: 3.0-3.5; Alpha-tocopherol acetate: 0.15; Propolis: 2; Calcium stearate: 0.92-0.95; Talc—3; Lactose—balance.

Leveton effect is caused by a synergism its ingredients:accurately dosed vitamins and phytoecdysteroid donors—rhaponticum carthamoides and pollen (pollen load).

The objective of Leveton development was the creation of such a preparation, the main action mechanism of which would be the effect on the processes of metabolism within cells. The preparation renders not only general strengthening and tonic effect on human body, but is also recommended for a preventive maintenance of the central nervous system dysfunction, treatment of prostate and erectile dysfunction.”

From the text of the patent RU 2,233,666, “APILAR” tablets contain: “The tablets having an anabolic and anticatabolic effect, wherein said tablets contain adsorbed homogenate of drone brood (homogenate, lactose, pectin, preservatives—sorbic and citric acids), as well as calcium stearate and flavorant as auxiliary substances at the following ingredient ratio in tablet mass per 100 tablets, g: Drone brood homogenate: 12.0-14.5; Lactose: 30.0-38.0;Pectin: 3.0-5.0;Sorbic acid: 0.1-0.4; Citric acid: 0.03-0.5; Sweetener: 0.05-0.5; Calcium stearate: 0.5-1.0; Flavorant: 0.1-0.5”

The prototypes have the following disadvantages: In R. D. Seifulla's patent RU 2,066,963, the preparation targets the general strengthening and tonic effect on a human body. According to the information presented in the source RU 2,066,963, no increase in muscular weight in athletes, maintenance of testosterone level, anabolic, anticatabolic or testosterone level effects were achieved in the source. In addition, according to the specified source of the information, the preparation proposed by R. D. Seifulla has substantial disadvantages, such as:

1) Allergic effect of pollen; 2) Rapid loss of the biological value of pollen during storage: a sharp decrease in activity versus time? As well as destructive temperature effect were observed. Existing preservation technologies cannot guarantee complete preservation of pollen ingredients. A part of vitamins and amino acids is already destroyed during the drying stage. Bees receiving pollen stored for a year in a refrigerator, have produced 56% less brood than those receiving fresh pollen, i.e. about half of the nutritious activity of flower pollen is lost.

3) Differences in chemical composition. Although Leveton is produced based on pollen collected from miscellaneous herbs, the chemical composition of pollen from batch to batch varies, which should be considered by a coach when prescribing Leveton.

4) Intake method. The most effective method of pollen intake is sublingually by the mouth, otherwise multiple useful substances contained in pollen are destroyed by digestive juices of the stomach. However, not all the people can tolerate such intake method.

Disadvantages of the APILAR tablets (RF Patent 2,233,666 by D. S. Lazaryan) are the following:

1) Short shelf life and refrigerator storage. This can be explained as follows: Drone brood deteriorates very quickly. If royal jelly is acidic (pH=3.5-4.5), and therefore, possesses bactericidal properties, drone brood is neutral (pH=6.11±0.11), and therefore deteriorates quickly. It can be stored for no longer than 1 hour. If used after that—one could get poisoned. (Krivtsov N. I. et al., Theory and means of apiotherapy. Publishing house OOO PKF “Komilfo”, 2007). Therefore, APILAR tablets are stored in a refrigerator and have a shelf life of 6 months.

2) It is necessary to note, that anabolic activity of APILAR tablets in the Patent 2,233,666 has a declarative nature (it is not confirmed by the information in the specification). Referring to the Table 1 of this patent, the gain of weight in the animals was as follows:

placebo: 15.91%;

Apilac: 22.98%;

APILAR tablets: only 13.53%.

i.e., less than in case of placebo. For that very reason, APILAR tablets have not found the application in sports.

Nowhere in the text of the RF Patent 2,233,666 or its specification there is a reference to: maintenance of testosterone level, anticatabolic and testosterone level effects.

The RF Patent 2,233,666 by D. S. Lazaryan has a priority date of December 30, 2002, and the RF Patent 2,066,963 by R. D. Seifulla has a priority date of Oct. 20, 1993.

Both prototypes have substantial disadvantages, which prevented their extended application in sports.

OBJECTS AND SUMMARY OF THE INVENTION

The product proposed by the applicant is free of the prototype disadvantages and also possesses the following pronounced effects: it increases the muscular weight in athletes, maintains testosterone level, and demonstrates anabolic, anticatabolic and potency enhancing effects.

The long-term experience of coaches and sports doctors in Russia did not result in development of a product, which would render the same effect on a human body.

The proposed product does not represent a sum of two previously known patents. Unlike the closest prototypes of the proposed invention—Patents 2,233,666 by Lazaryan (APILAR tablets) and 2,066,963 by R. D. Seifulla (Leveton tablets), the applicant managed to create the product having: the ability to increase the muscular weight in athletes, maintain testosterone level, and demonstrate anabolic, anticatabolic and potency enhancing effects, which could net be achieved from the use of two given patents.

The technical result of the invention is the increase of muscular weight in athletes, maintenance of testosterone level, and demonstration of anabolic, anticatabolic and potency enhancing effects.

It is necessary to note, that in the Patent 2,066,963, R. D. Seifulla knew about a possibility of using larvae, but has rejected the application thereof because. “during the period of its development, the quantity of ecdysteroids may vary every day by hundreds of times, which could substantially affect the biological activity of the preparation. This does not allow to produce more precise dosage and, hence, more precise standardization.”

Besides, the simple use of the two given patents was not possible because Rhaponticum carthamoides is collected in the fall or in the early spring, when bees still (or already) do not fly, and hence, do not produce drone brood. Therefore, the practical issue was to create such a product, which would allow to maintain biological properties of the drone brood for a long time, and would be convenient to use. For this reason there is no mentioning in the literature of combining drone brood with any other medicinal herb besides Rhaponticum carthamoides.

DETAILED DESCRIPTION OF THE INVENTION

Proposed product: Biologically active food additive, containing Rhaponticum carthamoides (or a medicinal herb containing ecdysteroids), ascorbic acid (vitamin C) and vitamin E, and vehicles (calcium stearate, talc, lactose), provided that said additive contains drone brood, at the following ingredient ratio (wt. %): Drone brood: 1-70; Rhaponticum carthamoides (or a medicinal herb containing ecdysteroids): 5-70; Ascorbic acid: 3.6-70; Vitamin E: 0.16-30; Vehicle—balance.

The explanation of the above composition is as follows:

Drone brood differs from the pollen in that:

1) It does not cause allergic reaction;

2) It is stable in terms of biological effect;

3) It contains a multiple functional groups of sulfide group enzymes, as well as hormones-testosteroids—progesterone and estradiol. Due to such set of substances, drone brood promotes accelerated recovery of biochemical and mass metric characteristics of seminal and prostate glands by acting as a stimulant of the central mechanisms of androgen formation intensity regulation.

Chemical composition: proteins: 10-20%; carbohydrates: 1-5.5%; fats: 5-6.3%; amino acids: 11.4%; glucose: 3.18-5%; fructose, sucrose: up to 0.5%.

Microelements (mg %): K—0.50; Na—38; Ca—14; P—189; Mg—2; Fe—3.23; Mn—4.40; Zn—5.54, Cu—2; Cr, Co, Ni, Ag, Au, etc.

Vitamins (water- and fat-soluble): A—0.54 I.U./g; xanthophyll—0.297 mg %; β-carotin—0.426 I.U./g; B2—0.739 mg %; D—950 I.U./g; choline—442.8 mg %; nicotinic acid—15.8 mg %.

Drone brood increases metabolism level during active muscular activity resulting in enhanced physical endurance. Drone brood contains 10 times more steroid hormones, than pollen.

As opposed to the prototypes, administration of increased doses of vitamins C and E is explained by enhancement of anticatabolic effect of the proposed product.

In the proposed invention, the antioxidant effect of the product is enhanced due to increase in the dose of vitamins C and E.

On page 14 of the book by T. V. Bubnova entitled “Allowed medicinal products and BAA—a guidance for body builders and weightlifters” (in Rus.), PGPU Methodical recommendations, it is stated: “During intensive physical activities, an accelerated break-down and elimination of vitamins from the body takes place, causing the need in them to increase. It is known, for example, that performance of moderate and heavy work . . . requires an increase in vitamin supply to the body by 1.5-3 times”.

The same book references the daily vitamin need for a body of a person not engaged in physical activities (Table 3, p. 15), as: Vitamin C—50-100 mg, and for a person engaged in physical activities (Table 4, p. 16), as: Vitamin C—120-250 mg”, i.e. in the known prototype the existing body need in vitamin C is not achieved. The suggested ratio in the proposed invention, on the other hand, provides antioxidant protection of the body exposed to increased loads.

It is also necessary to emphasize, that the presence of increased doses of vitamin C in the proposed invention is a mandatory condition, since vitamin C enables control of fluctuations of cortisone levels caused by weight training. Cortisone is a hormone that destroys muscles and is capable of turning metabolism in catabolic direction. Increased level of cortisone destroys muscular tissue.

Joint application of vitamins C and E enhances antioxidant and anticatabolic effect of these vitamins.

While searching the sources of scientific, technical and patent information, no substance was found that would possess a similar combination of essential features enabling the same positive effect. Thus, the proposed invention represents a technical solution to the problem demonstrating novelty, inventive level and industrial applicability. A therapeutic and preventive product is produced in the form of tablets. The lower limit is determined by convenience of use of the proposed complex, i.e. the use of lower quantity of tablets. The upper limit is determined by the fact that at a higher percentage ratio, it will be difficult to obtain a tablet: it will break up.

EXAMPLE 1

Example of the complex formulation for a 500 mg tablet:

-   Drone brood—10 mg; -   Rhaponticum carthamoides (or a medicinal herb containing     ecdysteroids)—50 mg; -   Ascorbic acid—50 mg; -   Vitamin E—5 mg; -   Vehicles—385 mg.

It is necessary to emphasize the role of vehicles in the proposed product. Without vehicles it would be impossible to create the proposed product and, in particular, combine Rhaponticum carthamoides and drone brood. The specified ascorbic acid and vehicle content allowed to achieve preserving effect, while retaining all properties of Rhaponticum carthamoides and drone brood.

Thus, the proposed biologically active additive created based on Rhaponticum carthamoides (or a medicinal herb containing ecdysteroids), drone brood, ascorbic acid (vitamin C), vitamin E, and vehicles can be used as a means for building up muscular weight in athletes due to increased content of phytoecdysteroids, which are phytohormones affecting anabolic processes in the athlete's body.

The preparation renders not only anabolic effect on a human body, but is also recommended for prevention of the central nervous system dysfunction, as well as treatment of prostate disease and erectile dysfunction.

The use of the proposed product reliably promotes anticatabolic processes in the muscular tissue for types of sports characterized by building endurance. Portugalov S. N. has studied the effect of the proposed product on Mordovian race walkers during training camp in Adler. The walkers specialize in race walking the distance of 20 and 50 km. This category of athletes does not require the growth of muscular weight. He has found that:

THE EFFECT OF THE “proposed product” ON THE BODY COMPOSITION PARAMETERS DURING BODY FAT ASSESSMENT TEST WERE AS FOLLOWS.

Param- Before use After use eters Test Check Test Check Body 65.8 ± 0.4 66.1 ± 0.25 64.6 ± 0.2  64.8 ± 0.4 weight, kg Muscle 34.15 ± 0.16 34.23 ± 0.12  33.99 ± 0.10 * 32.48 ± 0.20 weight, kg % 51.9 ± 0.1 51.8 ± 0.1  51.7 ± 0.2 * 50.9 ± 0.4 Fat  5.85 ± 0.12 5.9 ± 0.2 5.29 ± 0.24   5.57 ± 0.20 weight, kg %  8.9 ± 0.1  9.4 ± 0.12 8.29 ± 0.2   8.6 ± 0.16 * Deviations between the test and control were statistically insignificant.

The variation in the athletes overall testosterone blood level before and after the experimental education and training camp.

Group Initial level Final level Control M 22.4 ± 0.8 M18.6 ± 1.0 (p < 0.05) F 3.6 F 2.1 Test M 20.9 ± 0.4 M19.8 ± 0.8 (p > 0.05) F 2.4 F 2.5

Conclusion based on conducted study: “Effect of the “proposed product” on athlete body load adaptation characteristics. The level of adaptation in track-and-field athletes/runners with respect to endurance was assessed based on dynamics of biochemical control characteristics of blood during training. Within the scope of this study, the control of biochemical characteristics was conducted based on testing athletes blood samples drawn in the morning on an empty stomach after the day of resting. In the blood samples, the quantitative content of the following parameters was determined: HB, urea, lactate, glucose, Mg, P, testosterone.

As a result of conducted measurements, the following has been determined:

-   -   No reliable differences were established between the athletes of         the test group and control group with respect to the dynamics of         the levels of HB, urea, lactate, glucose, Mg, and P.     -   The testosterone level in athletes of the control group         decreased by the average of 16.9% (p<0.05) by the end of the         education and training camp.     -   Unlike the control group, no reliable variation of testosterone         level was detected in athletes of the test group during the same         time period (Tabl. 4).

It is important to note that the study was conducted under RUSADA supervision”.

It is important that nothing about testosterone level studies or the effect of Leveton or Apilar on human testosterone level was mentioned in either of the patents 2,233,666 or 2,066,963.

For the first time, the applicant managed to create a product rendering strong effect on human testosterone level without the use of the doping means, which has ensured the anabolic, anticatabolic and potency enhancing effects.

The applicant has conducted the studies to establish the effect of the proposed product on testosterone level. The following compositions were selected for the study:

Active ingredient content in the “Proposed Product 1”

Ingredients mg Rhaponticum carthamoides 100 Drone brood 100 Vitamin C 30 Vitamin E 3

Active ingredient content in the “Proposed Product 2”

Ingredients mg Rhaponticum carthamoides 50 Drone brood 50 Vitamin C 30 Vitamin E 3

The clinical study was conducted in 30 males with erectile dysfunction. The inclusion criteria were age-related:—Age 19-60 (sampling restriction based on age is associated with frequent detection in males older than 60 of the pronounced organic brain and somatic pathology, as well as paracmastic processes);—Consistence of the patient condition at the time of inclusion with the ICD-10 diagnostic criteria for F52.2—Failure of genital response, accompanied by one of following neurotic disorders: phobic anxiety disorders (F40); mixed manic depressive disorder (F41.2) and adjustment disorder (F43.2);—Absence of leading organic pathology in sexual disorder pathogenesis.

The study did not include patients with alcoholism; drug addiction; anatomic penis deformations; confirmed endocrine ED causes; decompensated somatic diseases; use of other means of ED treatment and preparations capable of causing ED.

All the patients have signed the informed consent form to participate in the study.

To realize the study objectives, the patients were distributed into 3 therapeutic groups based on the simple randomization method—two test groups and one control group:

-   Group 1. Test group—12 patients with erectile dysfunction and     combined psycho-emotional disorders, receiving “Proposed product 1”     along with conventional psycho-pharmacotherapy. -   Group 2. Test group—13 patients with erectile dysfunction and     combined psycho-emotional disorders, receiving “Proposed product 2”     along with conventional psycho-pharmacotherapy. -   Group 3. Control group consists of 5 patients with erectile     dysfunction and combined psycho-emotional disorders, receiving     conventional psycho-pharmacotherapy.

For the duration of 4 weeks the preparation “Proposed product 1” and “Proposed product 2” was prescribed in a dose of 2 tablets twice a day 30 minutes before meals. The assessment of therapy results was conducted on Day 28 of the treatment. Restoration of sexual life was considered as the main criterion of the treatment efficacy.

By Day 7 since the start of therapy using preparations “Proposed product 1” and “Proposed product 2” in both test groups the patients have already noted subjective mood improvement, increase in self-validation and confidence in their sexual potential, decrease in intensity and reduction in conflicts in their marital relations, as well as increase in frequency of spontaneous erections.

The study of the efficacy of the “Proposed product 1” and “Proposed product 2” relative to the sexual function of patients considering the clinical and dynamic variation of testosterone blood level has shown the following results (Table 3):

TABLE 3 Testosterone level dynamics since the beginning of therapy Average cumulative characteristics Group 1 (n = 12) Group 2 (n = 13) Day 28 after Day 28 after Group 3 (n = 5) Studied Before beginning of Before beginning of Before parameters treatment treatment treatment treatment treatment Day 28 Total 11.8 ± 4.4 14.6 ± 5.2 14.5 ± 4.7 17.3 ± 5.6 12.9 ± 4.7 13.1 ± 5.8 testosterone

In Group 1, where the preparation “Proposed product 1” was used, testosterone level increased by 23.7%, and in Group 2, where the preparation “Proposed product 2” was used, testosterone level increased by 19.8%.

By Day 28, an increase in sexual function parameters, such as sex drive and erection, during therapy using “Proposed product 1” and “Proposed product 2” was established in 66.7 and 61.5% of the patients, respectively. The average sex drive increase was 28.0 and 24.,3%, and erection increase—21.4 and 17.8%, respectively. In the Control group the fluctuations of testosterone level were insignificant.

It is necessary to note another important fact of using the proposed product—it is doping free. Extended use of the proposed product does not suppress production of its own hormones by the human body. The applicant has established that upon extended use of the proposed product, testosterone levels in human body reach reference values, at which point any further growth stops. Continuing use of the proposed product does not result in either increase or decrease in testosterone level.

Anticatabolic action of the proposed product has found widespread use among athletes—body builders, who actively use testosterone drugs (forbidden in official sports). These athletes develop a so-called “kickback” problem. After the use a course of “chemistry”, and specifically, exogenous testosterone drugs, an atrophy of male endocrine organs occurs. Therefore, there is an urgency in being able to rapidly restore such organs upon termination of steroid drug use, since at this time the body builder's body experiences low level of endogenous testosterone. As a result, catabolic processes start prevailing within the body leading to substantial drop in the muscular weight built up while using “chemistry”.

Application of the proposed product considerably accelerates the restoration of endogenous testosterone at athletes—body builders, which allows achieving more powerful results in preservation of the muscular weight after a course of “chemistry” compared to without application of the proposed product.

It is necessary to note that none of the prototypes had such an application.

Conducted preliminary observations among athletes (masters of sports, masters of sports of international level) taking the proposed product have shown its high efficacy relative to muscular weight build-up in comparison with Leveton (102%), Rhaponticum carthamoides (106%) and APILAR (drone brood (103%)), which is a very good result for highly qualified athletes. According to the order of the Ministry of Sports and Tourism regarding “weightlifting”, the following qualification norms were established for the “Masters of sports” title:

Weight category Norm, kg 77 kg 280 85 kg 295 94 kg 310 In other words, the difference is only 5%. Therefore, increase in performance by even 2% when using the proposed product is considered a fantastic result.

Average Average Average body weight, muscle weight, fat weight, Groups of athletes kg kg kg 1. Initially 92.30 58.04 9.2 1. After taking 92.66 59.00 8.6 APILAR (drone brood) 2. Initially 91.70 59.51 7.33 2. After taking 90.29 59.0 6.43 Rhaponticum carthamoides 3. Initially 90.1 57.75 8.11 3. After taking Leveton 89.45 58.10 7.11 4. Initially 85.3 56.06 6.9 4. After taking the 86.7 58.36 6.0 proposed PRODUCT

It is necessary to emphasize that the effect of the proposed product is provided by the entire combination of all the ingredients of the proposed product, which individually do not possess the proposed effect.

As a result, the proposed product has the following advantages compared to the prototypes:

1) an increase in shelf life of the product;

2) lower sensitivity to storage conditions;

3) convenience of use: can be swallowed or dissolved by sucking, while the prototype Leveton can only be dissolved sublingually.

4) proposal of the alternative composition compared to the existing preparations: someone may have allergy or intolerance toward pollen.

5) Stability of properties of the product as opposed to the prototypes.

6) Discovering new properties of the proposed product: anticatabolic, maintenance and/or restoration of testosterone level. 

I claim:
 1. A Biologically active food additive intended for increasing the muscular weight in athletes, maintaining testosterone level and demonstrating anabolic, anticatabolic and potency enhancing effects, comprising Rhaponticum carthamoides or a medicinal herb containing ecdysteroids, ascorbic acid, vitamin E, and vehicles, such as calcium stearate, talc, the lactose, wherein said additive contains drone brood at the following ingredient ratio (wt. %): Drone brood: 1-70; Rhaponticum carthamoides (or a medicinal herb containing ecdysteroids): 5-70; Ascorbic acid: 3.6-70; Vitamin E: 0.05-30; Vehicles—balance. 